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ESI-09 is a membrane-permeant inhibitor of both exchange proteins activated directly by cyclic AMP, Epac 1 and Epac 2. ESI-09 displays in vitro values of 3.2 μM for Epac 1 and 1.4 μM for Epac 2 with 25 μM cAMP as competing activator (Almahariq et al. 2013). It displays an at least 100-fold selectivity for Epac proteins compared to cyclic AMP-dependent protein kinase I and II in assays (Almahariq et al. 2013).
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RUO – Research Use Only |
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